2-bromo-5-methoxy-4,6-dimethylpyridine | 1062541-77-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-bromo-5-methoxy-4,6-dimethylpyridine
• 英文别名: 6-bromo-3-methoxy-2,4-dimethyl-pyridine；6-Bromo-3-methoxy-2,4-dimethylpyridine
• CAS: 1062541-77-8
• 化学式: C₈H₁₀BrNO
• 分子量: 216.077
• InChiKey: PENZXXCPRLNOBE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-bromo-5-methoxy-4,6-dimethylpyridine 在 三溴化硼 、 水 、 碳酸氢钠 作用下， 以 二氯甲烷 为溶剂， 反应 16.5h， 以78%的产率得到6-溴-2,4-二甲基-3-羟基吡啶
  参考文献：
  名称：

  [EN] COMPOUNDS COMPRISING A 3-PYRIDINOL OR 5-PYRIMIDINOL RING HAVING AN ORGANOSELENO OR ORGANOTELLURO SUBSTITUENT FOR USE AS ANTIOXIDANTS
  [FR] COMPOSÉS COMPRENANT UN NOYAU 3-PYRIDINOL OU 5-PYRIMIDINOL À SUBSTITUANT ORGANOSÉLÉNO OU ORGANOTELLURO UTILISÉS COMME ANTI-OXYDANTS

  摘要：

  含有3-吡啶醇或5-嘧啶醇环，在吡啶或嘧啶环上带有有机硒或有机碲取代基团的化合物，表现出有用的抗氧化性能。这些化合物可能符合以下定义的化学式(I)。还披露了催化链断裂和过氧化物分解抗氧化性能。此外，这些化合物可以与还原剂结合使用。这些化合物可用于稳定人造和天然材料，或用于预防或治疗由自由基介导或氧化组织损伤引起的疾病。

  公开号：

  WO2009144253A1
• 作为产物：
  描述：

  3-amino-2-bromo-5-methoxy-4,6-dimethylpyridine 在 tetrafluorohydroboric acid 、 sodium nitrite 、 phosphinic acid 作用下， 以 水 为溶剂， 反应 0.25h， 生成 2-bromo-5-methoxy-4,6-dimethylpyridine
  参考文献：
  名称：

  Catalytic Chain-Breaking Pyridinol Antioxidants

  摘要：

  When assayed for their capacity to inhibit azo-initiated peroxidation of linoleic acid in a water/chlorobenzene two-phase system, tellurium-containing 3-pyridinols were readily regenerable by N-acetylcysteine contained in the aqueous phase. The best inhibitors quenched peroxyl radicals more efficiently than alpha-tocopherol, and the duration of inhibition was limited only by the availability of the thiol reducing agent. The compounds were also found to catalyze reduction of hydrogen peroxide in the presence of thiol reducing agent.

  DOI：

  10.1021/ol801983n

文献信息

• NEW COMPOUNDS 574
  申请人：HOLENZ Jorg

  公开号：US20100125081A1

  公开（公告）日：2010-05-20

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

  本发明涉及具有式（I）的新化合物及其药物组合物。此外，本发明涉及治疗方法，用于治疗和/或预防与Aβ相关的病理学，如唐氏综合征、β-淀粉样蛋白血管病，如但不限于脑淀粉样蛋白血管病或遗传性脑出血，与认知损害相关的疾病，如但不限于MCI（“轻度认知损害”）、阿尔茨海默病、记忆丧失、与阿尔茨海默病相关的注意力缺陷症状，与疾病如阿尔茨海默病或痴呆症相关的神经退化，包括混合性血管性和退行性起源的痴呆、老年前期痴呆、老年痴呆和与帕金森病、进行性上丘脑麻痹或皮质基底节变性相关的痴呆。
• [EN] COMPOUNDS COMPRISING A 3-PYRIDINOL OR 5-PYRIMIDINOL RING HAVING AN ORGANOSELENO OR ORGANOTELLURO SUBSTITUENT FOR USE AS ANTIOXIDANTS<br/>[FR] COMPOSÉS COMPRENANT UN NOYAU 3-PYRIDINOL OU 5-PYRIMIDINOL À SUBSTITUANT ORGANOSÉLÉNO OU ORGANOTELLURO UTILISÉS COMME ANTI-OXYDANTS
  申请人：KAROLINSKA INST INNOVATIONS AB

  公开号：WO2009144253A1

  公开（公告）日：2009-12-03

  Compounds comprising a 3-pyridinol or 5-pyrimidinol ring carrying an organoseleno- or organotelluro- substituent on the pyridine or pyrimidine ring, exhibit useful antioxidant properties. The compounds may for example be in accordance with the following formula (I) as defined herein. Catalytic chain-breaking and hydroperoxide decomposing antioxidant properties are also disclosed. Furthermore the compounds may be used in combination with a reducing agent. The compounds are useful for the stabilization of man-made and natural materials, or for the prevention or treatment of disorders caused by or involving free radical-mediated or oxidative tissue damage.

  含有3-吡啶醇或5-嘧啶醇环，在吡啶或嘧啶环上带有有机硒或有机碲取代基团的化合物，表现出有用的抗氧化性能。这些化合物可能符合以下定义的化学式(I)。还披露了催化链断裂和过氧化物分解抗氧化性能。此外，这些化合物可以与还原剂结合使用。这些化合物可用于稳定人造和天然材料，或用于预防或治疗由自由基介导或氧化组织损伤引起的疾病。
• NEW COMPOUNDS 578
  申请人：HOLENZ Jörg

  公开号：US20100125082A1

  公开（公告）日：2010-05-20

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

  本发明涉及式(I)的新化合物及其药物组合物。此外，本发明涉及用于治疗和/或预防与Aβ相关的病理学，如唐氏综合症，β-淀粉样蛋白血管病，如但不限于脑淀粉样蛋白血管病或遗传性脑出血，与认知损害相关的疾病，如但不限于MCI（“轻度认知损害”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与疾病如阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合性血管性和退行性起源的痴呆，早老性痴呆，老年性痴呆和与帕金森病，进行性上核性麻痹或皮层基底变性相关的痴呆有关的治疗方法。
• NEW COMPOUNDS 575
  申请人：HOLENZ Jorg

  公开号：US20100125087A1

  公开（公告）日：2010-05-20

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

  本发明涉及式（I）的新化合物及其药物组成。此外，本发明涉及治疗方法，用于治疗和/或预防与Aβ相关的病理，如唐氏综合症、β-淀粉样蛋白血管病变，如但不限于脑淀粉样蛋白血管病变或遗传性脑出血，与认知受损相关的疾病，如但不限于MCI（轻度认知障碍）、阿尔茨海默病、记忆丧失、与阿尔茨海默病相关的注意力缺陷症状，与阿尔茨海默病或痴呆症等疾病相关的神经退行性疾病，包括血管性和退行性起源的混合性痴呆、早老性痴呆、老年痴呆和与帕金森病、进行性上核性麻痹或皮层基底节变性相关的痴呆。
• Substituted Isoindoles
  申请人：HOLENZ Jörg

  公开号：US20110319426A1

  公开（公告）日：2011-12-29

  The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

  本发明涉及式（I）的新型化合物及其制药组合物。此外，本发明涉及治疗和/或预防与Aβ相关的病理学，例如唐氏综合症、β-淀粉样蛋白血管病，例如脑淀粉样血管病或遗传性脑出血，与认知障碍有关的疾病，例如轻度认知障碍（MCI）、阿尔茨海默病、记忆丧失、与阿尔茨海默病相关的注意力缺陷症状、与阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合的血管性和退行性起源的痴呆症、老年前期痴呆症、老年痴呆症和与帕金森病、进行性核上性麻痹或皮质基底节变性有关的痴呆症的治疗方法。